Cas No.: | 91917-65-6 |
Chemical Name: | RO 15-4513 |
Synonyms: | RO 15-4513;ethyl 8-azido-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate;8-Azido-5,6-dihydro-5-Methyl-6-oxo-4H-iMidazo[1,5-a][1,4]benzodiazepine-3-carboxylicacidethylester;Ethyl-8-azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazo-1,4-benzodiazepine-3-carboxylate;Tocriscreen Total |
SMILES: | [N-]=[N+]=NC1C=CC2N3C=NC(C(OCC)=O)=C3CN(C(=O)C=2C=1)C |
Formula: | C15H14N6O3 |
M.Wt: | 326.31006193161 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR)[1]. Ro15-4513 is a potent ethanol antagonist[2]. Ro15-4513 has anti-anxiety effect[3]. |
Target: | BZR[1]; ethanol[2]; |
In Vivo: | Ro 15-4513 (i.p.; 3 mg/kg; 10 min before being tested) completely inhibits the ethanol-induced (1.8 g/kg) reduction in total locomotor activity and partly the reduction in rearing[2]. Ro 15-4513 (i.p.; 3 mg/kg; 15 min before administration of 1.5 g/kg ethanol) reverses ethanol-induced sedation in GABAA receptor δ subunit-deficient mice[2]. Animal Model: Male C57BL/6J mice[2] Dosage: 3 mg/kg Administration: I.p.; 10 min before being tested Result: Completely inhibited the ethanol-induced reduction in total locomotor activity and partly the reduction in rearing. |
In Vitro: | Ro15-4513 usually acts as a partial inverse agonist at GABAA receptors, except an agonist for α4 and α6 subunit-containing ones[3]. |
References: | [1]. Bonetti EP, et al. Ro 15-4513: partial inverse agonism at the BZR and interaction with ethanol. Pharmacol Biochem Behav. 1988 Nov;31(3):733-49. [2]. Suzdak PD, et al. Effects of Ro15-4513 and other benzodiazepine receptor inverse agonists on alcohol-inducedintoxication in the rat. J Pharmacol Exp Ther. 1988 Jun;245(3):880-6. [3]. Linden AM, et al. Ro 15-4513 Antagonizes Alcohol-Induced Sedation in Mice Through αβγ2-type GABA(A) Receptors. Front Neurosci. 2011 Jan 20;5:3. |